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ZA99161B - Ó-ketoamide inhibitors of 20S proteasome. - Google Patents

Ó-ketoamide inhibitors of 20S proteasome.

Info

Publication number
ZA99161B
ZA99161B ZA9900161A ZA99161A ZA99161B ZA 99161 B ZA99161 B ZA 99161B ZA 9900161 A ZA9900161 A ZA 9900161A ZA 99161 A ZA99161 A ZA 99161A ZA 99161 B ZA99161 B ZA 99161B
Authority
ZA
South Africa
Prior art keywords
proteasome
ketoamide inhibitors
ketoamide
inhibitors
Prior art date
Application number
ZA9900161A
Inventor
Lisa Wang
Robert T Lum
Steven R Schow
Alison Joly
Suresh Kerwar
Michael M Wick
Original Assignee
Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Therapeutics Inc filed Critical Therapeutics Inc
Publication of ZA99161B publication Critical patent/ZA99161B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA9900161A 1998-01-26 1999-01-11 Ó-ketoamide inhibitors of 20S proteasome. ZA99161B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/013,365 US6075150A (en) 1998-01-26 1998-01-26 α-ketoamide inhibitors of 20S proteasome

Publications (1)

Publication Number Publication Date
ZA99161B true ZA99161B (en) 1999-07-28

Family

ID=21759598

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA9900161A ZA99161B (en) 1998-01-26 1999-01-11 Ó-ketoamide inhibitors of 20S proteasome.

Country Status (20)

Country Link
US (2) US6075150A (en)
EP (1) EP1058689A1 (en)
JP (1) JP3863370B2 (en)
KR (1) KR100417888B1 (en)
CN (1) CN1289340A (en)
AR (1) AR012781A1 (en)
AU (1) AU747835B2 (en)
BR (1) BR9907256A (en)
CA (1) CA2319150C (en)
GE (1) GEP20032869B (en)
HU (1) HUP0100901A3 (en)
IL (2) IL137475A0 (en)
NO (1) NO327049B1 (en)
NZ (1) NZ505892A (en)
PL (1) PL202504B1 (en)
RU (1) RU2192429C2 (en)
TW (1) TW593339B (en)
UA (1) UA71559C2 (en)
WO (1) WO1999037666A1 (en)
ZA (1) ZA99161B (en)

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US6844315B2 (en) 1998-05-20 2005-01-18 Erasmus Universiteit Rotterdam Immunoregulator
US20030220258A1 (en) * 2001-12-21 2003-11-27 Robbert Benner Treatment of ischemic events
US6921751B1 (en) * 1998-05-20 2005-07-26 Erasmus Universiteit Rotterdam Immunoregulator
US20050227925A1 (en) * 2004-04-08 2005-10-13 Robbert Benner Compositions capable of reducing elevated blood urea concentration
US8680059B2 (en) * 1998-05-20 2014-03-25 Biotempt B.V. Oligopeptide acetate and formulations thereof
US20040202645A1 (en) * 2003-04-08 2004-10-14 Khan Nisar Ahmed Administration of gene-regulatory peptides
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
EP1300418A1 (en) * 2001-10-04 2003-04-09 Erasmus Universiteit Rotterdam Gene regulation by oligopeptides
US7358330B2 (en) 2001-03-29 2008-04-15 Biotempt B.V. Immunoregulatory compositions
WO2002070467A1 (en) * 2001-02-26 2002-09-12 4Sc Ag Derivatives of diphenylurea, diphenyloxalic acid diamide and diphenylsulfuric acid diamide and their use as medicaments
US20080242837A1 (en) * 2001-12-21 2008-10-02 Khan Nisar A Peptide compositions
US7501391B2 (en) * 2001-12-21 2009-03-10 Biotempt B.V. Treatment of transplant survival
US20030220257A1 (en) * 2001-12-21 2003-11-27 Robbert Benner Treatment of trauma
US20040013661A1 (en) * 2001-12-21 2004-01-22 Gert Wensvoort Stratification
US20030220260A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Peptide compositions
US20030220261A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Treatment of iatrogenic disease
US20080318871A1 (en) * 2001-12-21 2008-12-25 Khan Nisar A Treatment of neurological disorders
US7560433B2 (en) 2001-12-21 2009-07-14 Biotempt B.V. Treatment of multiple sclerosis (MS)
US7786084B2 (en) * 2001-12-21 2010-08-31 Biotempt B.V. Treatment of burns
US7282512B2 (en) 2002-01-17 2007-10-16 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
CA2481369C (en) * 2002-04-11 2012-07-10 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
US20090227505A1 (en) * 2004-01-07 2009-09-10 Biotempt B.V. Methods and uses for protein breakdown products
SG185963A1 (en) * 2004-05-10 2012-12-28 Onyx Therapeutics Inc Compounds for enzyme inhibition
EP1637529A1 (en) 2004-09-20 2006-03-22 4Sc Ag Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US20070027067A1 (en) * 2005-05-13 2007-02-01 Felicia Etzkorn Transition-state Inhibitors of Pin1, alpha-Ketoamide-containing peptidomimetics, and synthesis thereof
SG163567A1 (en) * 2005-07-05 2010-08-30 Biotempt Bv Treatment of tumors
DK1912997T3 (en) 2005-07-29 2012-01-02 Tibotec Pharm Ltd Macrocyclic inhibitors of hepatitis C virus
US8183277B2 (en) 2005-07-29 2012-05-22 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis C virus
US7687456B2 (en) 2005-11-09 2010-03-30 Proteolix, Inc. Compounds for enzyme inhibition
US8594771B2 (en) * 2005-12-28 2013-11-26 General Electric Company Devices and methods for self-administered ECG examinations
EP1864692A1 (en) * 2006-06-07 2007-12-12 Biotempt B.V. Use of peptides for the control of radiation injury
EP2484688B1 (en) 2006-06-19 2016-06-08 Onyx Therapeutics, Inc. Peptide epoxyketones for proteasome inhibition
WO2008100140A1 (en) * 2007-02-12 2008-08-21 Biotempt B.V. Treatment of trauma hemorrhage with short oligopeptides
US8859021B2 (en) * 2007-05-14 2014-10-14 Sytheon Skin appearance through gene manipulation
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
MX2010003732A (en) * 2007-10-04 2010-08-09 Onyx Therapeutics Inc Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides.
BR122014008753A2 (en) 2008-06-17 2015-12-29 Millennium Pharm Inc boronate ester compounds and pharmaceutical compositions thereof
PE20120059A1 (en) 2008-10-21 2012-02-27 Onyx Therapeutics Inc PHARMACEUTICAL COMBINATIONS WITH PEPTIDIC EPOXYCETONES
WO2010096574A1 (en) 2009-02-20 2010-08-26 Lisanti Michael P A method of diagnosis or prognosis of a neoplasm comprising determining the level of expression of a protein in stromal cells adjacent to the neoplasm
TWI504598B (en) 2009-03-20 2015-10-21 Onyx Therapeutics Inc Crystalline tripeptide ketone ketone protease inhibitor
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
CN102725300B (en) 2009-12-22 2015-03-11 赛福伦公司 Proteasome inhibitors and processes for their preparation, purification and use
US9359398B2 (en) 2010-03-01 2016-06-07 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
WO2011136905A2 (en) 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
SI2742356T1 (en) 2011-08-11 2016-06-30 Janssen Pharmaceutica N.V. Predictors for cancer treatment
CA2853822A1 (en) 2011-10-28 2013-05-02 Millennium Pharmaceuticals, Inc. Biomarkers of response to nae inhibitors
US20150184246A1 (en) 2011-11-11 2015-07-02 Millennium Pharmaceuticals, Inc. Biomarkers of response to proteasome inhibitors
CA2862492A1 (en) 2012-01-24 2013-08-01 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
US10085987B2 (en) 2012-01-27 2018-10-02 Thomas Jefferson University MCT protein inhibitor-related prognostic and therapeutic methods
US9309283B2 (en) 2012-07-09 2016-04-12 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
CA2886783A1 (en) 2012-10-01 2014-04-10 Millennium Pharmaceuticals, Inc. Biomarkers and methods to predict response to inhibitors and uses thereof
HK1212997A1 (en) * 2012-10-11 2016-06-24 F. Hoffmann-La Roche Ag Ketoamide immunoproteasome inhibitors
EP2986290A4 (en) 2013-04-19 2017-01-04 Thomas Jefferson University Caveolin-1 related methods for treating glioblastoma with temozolomide
CN106659761A (en) 2014-05-20 2017-05-10 千年药物公司 Boron-containing proteasome inhibitors for use after primary cancer therapy
JP6859559B2 (en) * 2017-03-16 2021-04-14 二村 芳弘 Phenyl peptide derivative with anti-allergic effect
US11667945B2 (en) 2017-08-28 2023-06-06 Shizuoka Prefecture Public University Corporation Detection method and detection probe for colibactin and colibactin-producing bacteria

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IT1206078B (en) * 1987-06-03 1989-04-14 Polifarma Spa PROCEDURE FOR THE PRODUCTION OF 3-INDOLPIRUVIC ACID AND ITS DERIVATIVES THEIR PHARMACEUTICAL USE
JPH04211648A (en) * 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd Keto-acid amide derivative
US5430022A (en) * 1990-05-14 1995-07-04 Fujisawa Pharmaceutical Co., Ltd. Peptide compound and its preparation
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6660268B1 (en) * 1994-03-18 2003-12-09 The President And Fellows Of Harvard College Proteasome regulation of NF-KB activity
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5834487A (en) * 1996-09-24 1998-11-10 Cv Therapeutics Inhibition of 26S and 20S proteasome by indanones

Also Published As

Publication number Publication date
JP3863370B2 (en) 2006-12-27
NO20003807D0 (en) 2000-07-25
HUP0100901A2 (en) 2001-08-28
HUP0100901A3 (en) 2001-11-28
KR20010034381A (en) 2001-04-25
IL137475A (en) 2006-10-05
US6075150A (en) 2000-06-13
CA2319150A1 (en) 1999-07-29
CN1289340A (en) 2001-03-28
AR012781A1 (en) 2000-11-08
NO327049B1 (en) 2009-04-14
WO1999037666A1 (en) 1999-07-29
KR100417888B1 (en) 2004-02-11
TW593339B (en) 2004-06-21
NZ505892A (en) 2002-10-25
BR9907256A (en) 2001-10-09
EP1058689A1 (en) 2000-12-13
NO20003807L (en) 2000-09-25
UA71559C2 (en) 2004-12-15
CA2319150C (en) 2004-08-31
JP2002501080A (en) 2002-01-15
RU2192429C2 (en) 2002-11-10
PL343269A1 (en) 2001-08-13
GEP20032869B (en) 2003-01-27
IL137475A0 (en) 2001-07-24
AU747835B2 (en) 2002-05-23
PL202504B1 (en) 2009-06-30
US6781000B1 (en) 2004-08-24
AU2326799A (en) 1999-08-09

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